20 results about "Fluconazole" patented technology

The invention relates to the technical field of medicines, in particular to application of tedizolid combined with fluconazole in preparation of antifungal drugs. The tedizolid and the fluconazole are combined for use, so that the antibacterial activity of the fluconazole on the candida albicans can be enhanced, a synergistic antifungal effect can be generated, and the drug resistance of the candida albicans on the fluconazole can be reversed.

The present invention relates to methods and means for inhibiting or preventing the growth of fungal cells with at least one flavone selected from the group consisting of 5-methoxyflavone, 2′-methoxyflavone, 7-methoxyflavone, 3′,4′,5,7-tetrametoxyflavone, 3′,4′,5′,5,6,7-hexymethoxyflavone, 7,8-benzoflavone and 5,6-benzoflavone for inhibiting or preventing the growth of a fungal cell, wherein said flavone is used in combination with at least one further antimycotic compound selected from the group of azoles, both in an amount to exhibit a synergistic effect compared to the separate use of said flavone and said antimycotic compound.

The application provides a long-acting external use efinaconazole composition, a preparation method and application, and belongs to the technical field of pharmaceutical compositions.The long-acting external use efinaconazole composition comprises the following components in percentage by weight: efinaconazole 0.5-3%, a film forming agent 3-7%, a gel agent 2-3%, a plasticizer 3-7%, a cosolvent 0.78-1.56% and a solvent in a residual amount.The application forms a eutectic mixture of efinaconazole and lactic acid, improves the solubility and permeability of the active ingredient, dissolves in the solvent of an ethanol system, and adds the film forming agent and the plasticizer, so that a drug depot is formed on the surface of the skin through the film forming principle, the drug is released slowly, the clinical compliance is improved, the frequency of drug administration is reduced, the bioavailability of the drug in the stratum corneum is increased, the effectiveness and safety of the drug can be improved, the basic theory of pharmacoeconomics is met, and the clinical value of the product is improved.

The invention discloses skin mucosa maintenance liquid capable of killing fungi and HPV (human papillomavirus) as well as a preparation method and application of the skin mucosa maintenance liquid, and belongs to the technical field of sterilization and virus removal. The skin mucosa maintenance liquid is prepared from octanol ether, benzalkonium bromide, phenoxyethanol, yermate, parachlorometaxylenol, taetinic acid, chitosan, keratinase, fluconazole, glycerol, borneol, menthol, absolute ethyl alcohol and tween-40. Wherein the skin mucosa maintenance liquid has an effect of regulating apoptosis induction on abnormal cells and an effect on vaginal flora, and has an obvious inhibition effect on cervicitis and colpitis mycotica, namely an anti-inflammatory effect; meanwhile, apoptosis of cells containing HPV16 and HPV18 genes can be induced, shedding of abnormal cells is promoted, diseased cells are killed, and vaginal tissues with pathological changes are removed.

This invention discloses an antimicrobial peptide, its pharmaceutical composition, and its applications. The invention optimizes the structure of the antimicrobial peptide through deuteration modification technology, significantly enhancing its targeted binding ability to β-1,3-D-glucan synthase. The affinity of this antimicrobial peptide for the aforementioned target is 9-27 times that of the control peptide. In vitro assays show that its minimum inhibitory concentration (MIC) against nine standard Candida strains is consistently 0.002 μg / mL, exhibiting significantly superior activity compared to fluconazole, anidoxurine, and the control peptide. It also exhibits extremely low cytotoxicity against L02 human normal hepatocytes. In in vivo experiments, in a neutropenic mouse model of Candida albicans infection, the antimicrobial peptide at all doses showed superior reduction in renal fungal load compared to anidoxurine and the control peptide. The antimicrobial peptide of this invention combines highly efficient anti-Candida activity, low cytotoxicity, and excellent in vivo efficacy, providing a safe and effective candidate drug for the treatment of drug-resistant candidiasis and possessing good clinical translational value.

This application relates to the field of biotechnology, and particularly to primer pairs, primer-probe compositions, PCR premixes, kits, and methods for detecting multiple respiratory pathogens. Nucleic acid sequences are shown in primer pairs as indicated by SEQ ID NO: 1-2, 4-5, 7-8, 10-11, 13-14, 16-17, 19-20, 22-23, 25-26, 28-29, 31-32, 34-35, 37-38, and 40-41. For target respiratory pathogens, this application designs specific amplification primer pairs, paired with suitable probes, enabling the simultaneous detection of eight targets. Furthermore, the detection process avoids interference from heme, trimethoprim, sulfamethoxazole, amphotericin B, itraconazole, fluconazole, azithromycin, adrenaline, and lidocaine hydrochloride in the test sample. It exhibits good anti-interference properties and shows no cross-reactivity with *Rhodococcus equi*, *Candida tropicalis*, and *Candida krusei*.

The application discloses a long-chain non-coding RNA of Candida albicans for epigenetically regulating fluconazole resistance and application thereof, belongs to the technical field of biological medicines, and relates to antifungal medicines. The long-chain non-coding RNA for epigenetically regulating fluconazole resistance comprises three nucleotide sequences shown in SEQ ID NO. 1-3. The application further provides application of Momordica charantia protein MAP30 in inhibiting expression of the long-chain non-coding RNA of the Candida albicans genome. The application provides nucleotide sequencing of the long-chain non-coding RNA of the Candida albicans genome for epigenetically regulating fluconazole resistance, open reading frame (ORF) alignment, positioning of the lncRNA on a chromosome, inhibition of lncRNA expression by using the Momordica charantia protein MAP30, and realization of reversing fluconazole resistance, which provides a theoretical basis for revealing the Candida albicans resistance mechanism, developing new antifungal medicines and treatment strategies.

The application discloses an antifungal azole derivative, a synthesis method and application thereof, and has a general formula shown in formula (I). The azole derivative is synthesized by recombination of fluconazole and ketoconazole structural units, and the application of the azole derivative provided by the application is the application in preparation of antifungal drugs. The azole derivative synthesized by the application is superior to fluconazole (FLC) in inhibiting effect on Candida albicans, and the MIC 50 value can be as low as 0.0218 μg / mL, thereby providing a new direction for research and preparation of an antifungal drug for Candida albicans.

The application discloses fluconazole ear drops and a preparation method thereof, and belongs to the technical field of ear drop preparations. The fluconazole ear drops contain the following components in percentage by mass: 0.6%-2.0% of fluconazole, 8%-20% of propylene glycol and / or diethylene glycol monoethyl ether, 20%-32% of glycerol or capryl capric acid polyethylene glycol glycerol ester, 0.1%-1% of hydroxypropyl methyl cellulose, 0.05%-0.2% of anhydrous disodium hydrogen phosphate, and water in a residual amount. The solubility of fluconazole is increased through improvement of the prescription of the fluconazole ear drops, the content of fluconazole in the prepared fluconazole ear drops reaches 2%, and the fluconazole ear drops have good stability. Compared with the prior art, the fluconazole ear drops have a better treatment effect on ear fungal infections.

Disclosed in the present invention are antifungal compounds, a preparation method therefor, and the use thereof. The compounds have the following general formula I, wherein L represents a linking moiety, referring to a small molecule fragment, and Ar represents a heterocyclic ring or a substituted heterocyclic ring. The series of compounds of the present invention can better bind to an enzyme target by means of various interaction forces, thereby exhibiting good activity; and the compounds exhibit excellent activity in both in vitro experiments and animal experiments, the activity of most of the compounds against Candida albicans being better than that of fluconazole. In addition, the series of compounds have anti-inflammatory effects while eliminating fungal infections; and compared with voriconazole, the series of compounds of the present invention can remarkably down-regulate the expression of an inflammatory factor interleukin 6.

The invention discloses a verification method and application of an ADH2 gene in systemic Candida albicans infection treatment, and belongs to the technical field of microbial medicine and anti-infection treatment. The verification method comprises the following steps: constructing an ADH2 single allele knockout strain and an ADH2 double allele knockout strain by taking wild type candida albicans SC5314 as a starting strain, and evaluating the effectiveness of an ADH2 target spot through body and appearance verification, in-vitro metabolism verification, in-vitro drug sensitivity verification and immunosuppression mouse in-vivo pathogenicity and curative effect verification. In the application aspect, the medicine for treating systemic Candida albicans infection is prepared by regulating and controlling the function of the ADH2 gene in the Candida albicans, the abnormal metabolism of a biological membrane caused by function imbalance of the ADH2 can be corrected, and the sensitivity of the Candida albicans to fluconazole is enhanced or the toxicity of the Candida albicans is reduced. The invention provides a new intervention way for the drug resistance problem of the antifungal drug, and provides technical support for research and development of the antifungal drug.

This invention relates to the field of pharmaceutical technology, specifically to the application of dehydronuciolin and fluconazole in the preparation of antifungal drugs. The in vitro synergistic effect of the combination of dehydronuciolin and fluconazole was determined using a checkerboard assay, showing a fractional inhibitory concentration (FIC) ≤0.5, confirming a strong synergistic effect. The in vivo efficacy of this drug combination was verified using a large wax moth infection model. Phenotypic experiments explored the synergistic mechanism, showing that the combination of dehydronuciolin and fluconazole significantly inhibited the hyphal growth, biofilm formation, and adhesion to host cells of drug-resistant Candida albicans. Transcriptome sequencing analysis confirmed these findings, showing that treatment with the combination of dehydronuciolin and fluconazole downregulated hyphae-specific genes, GPI-anchored cell wall proteins, and the ergosterol biosynthesis pathway, collectively weakening the virulence, surface integrity, and host recognition ability of Candida albicans, thereby reversing its drug resistance.

The invention provides a pramoxine hydrochloride and fluconazole combined pharmaceutical composition for resisting candida albicans biofilm infection and application of the pharmaceutical composition, and belongs to the technical field of biological medicine. Aiming at the problem of inherent drug resistance of a candida albicans biological membrane to azole drugs, drug relocation strategy screening finds that pramoxine hydrochloride can significantly enhance the inhibitory activity of fluconazole to the candida albicans biological membrane. The action mechanism is as follows: pramoxapine hydrochloride is specifically targeted to key protein mevalonate kinase in a farnesyl pyrophosphate synthesis route in candida albicans, biosynthesis of ubiquinone is inhibited, the active oxygen level of mitochondria is increased, the mitochondrial function is destroyed, the hypha length, the biological membrane thickness and extracellular matrix secretion of candida albicans are reduced, and the activity of pramoxapine hydrochloride in the candida albicans is improved. And finally, the anti-biofilm effect of fluconazole is improved. The invention provides a safe and efficient new strategy for resisting Candida albicans biofilm infection, and provides a new pharmaceutical composition and an action target for clinical treatment of biofilm related fungal infection.

The invention provides a triamino-substituted s-triazine compound as well as a preparation method and application thereof, and belongs to the field of medicines. The structural formula of the triamino-substituted s-triazine compound is as shown in formula I, wherein R is C6-C10 aryl or C6-C10 aryl substituted by one or more R1; each R1 is respectively and independently halogen,-CF3,-NO2,-CN, C1-C6 alkyl,-O-C1-C6 alkyl, C1-C6 alkyl substituted by one or more R1-1, or-O-C1-C6 alkyl substituted by one or more R1-2; in the formula (1), each R1 is independently halogen,-CF3,-NO2,-CN, C1-C6 alkyl,-O-C1-C6 alkyl, or-O-C1-C6 alkyl substituted by one or more R1-2; each R1-1 is each independently a halogen or a C6-C10 aryl group; each of R1-2 is independently a halogen; n is 0, 1 or 2; x is S or O atom; r1 and R2 are respectively and independently halogen. The compound is good in antifungal activity, and has an obvious synergistic antifungal effect when being used together with fluconazole.

The present application provides a kind of fluconazole-silicone foam dressing for incontinence dermatitis protection and its preparation method, the dressing is sequentially waterproof breathable backing layer, fluconazole-containing silicone modified polyurethane foam liquid-absorbing layer, silicone gel skin contact layer from outside to inside;In liquid-absorbing layer, fluconazole is loaded on mesoporous silica nanospheres, and the surface of microsphere is grafted with silicone modified polymer, and the silicone grafting rate of foam liquid-absorbing layer is 8%~15%.The present application has the advantages of high-efficiency liquid absorption, low hardness after liquid absorption, pH targeted drug release, no silicone migration and precipitation, no adhesion and easy removal, can effectively prevent incontinence dermatitis, inhibit secondary fungal infection, reduce secondary skin damage, and meet the clinical incontinence care needs.

The invention discloses an antibacterial peptide as well as a pharmaceutical composition and application thereof. The structure of the antibacterial peptide is optimized through a deuterated modification technology, and the targeted binding capacity of the antibacterial peptide to beta-1, 3-D-glucan synthetase is remarkably improved. The affinity of the antibacterial peptide to the target spot is 9-27 times that of a control peptide; in-vitro determination shows that the minimum inhibitory concentration (MIC) of the compound to nine standard candida strains is stabilized to be 0.002 mu g / mL, and the activity of the compound is remarkably superior to that of fluconazole, anidulafungin and control peptide; the cytotoxicity to L02 human normal hepatocytes is extremely low; in an in-vivo experiment, in a neutrophile granulocyte reduction mouse Candida albicans infection model, the kidney fungal load reduction effect under each dose of the antibacterial peptide is better than that of anidulafungin and a control peptide. The antibacterial peptide has efficient anti-candida activity, low cytotoxicity and excellent in-vivo curative effect, provides a safe and effective candidate drug for treatment of drug-resistant candidiasis, and has good clinical transformation value.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of R, S diastereoisomers of efinaconazole and intermediates of the R, S diastereoisomers. The efinaconazole diastereoisomer preparation method comprises the following steps: taking a compound 1 as a starting material, and carrying out oxidation reaction to obtain a compound 1-L; performing reduction reaction on the compound 1-L to obtain a compound 4; performing nucleophilic substitution reaction on the compound 4 to obtain a compound 4-1; and carrying out nucleophilic addition reaction on the compound 4-1 to obtain a compound 4-2. Compared with the prior art, the invention makes up the blank of the prior art, provides the preparation method of the S, R diastereoisomers of efinaconazole and the intermediates thereof, and provides help for drug research; the method has the advantages of mild reaction conditions, cheap and easily available reagents, low economic and time cost, no need of resolution, and high optical purity of the prepared product.

The invention relates to the technical field of biology, in particular to a primer pair, a primer probe composition, a PCR premix, a kit and a method for detecting multiple respiratory pathogens. The invention discloses a primer pair with nucleic acid sequences as shown in SEQ ID NO: 1-2, 4-5, 7-8, 10-11, 13-14, 16-17, 19-20, 22-23, 25-26, 28-29, 31-32, 34-35, 37-38 and 40-41. Aiming at a target respiratory pathogen, a specific amplification primer pair is designed and is matched with a proper probe, so that eight-target joint detection can be realized, and the influence of heme, trimethoprim, sulfamethoxazole, amphotericin B, itraconazole, fluconazole, azithromycin, epinephrine and lidocaine hydrochloride in a detection sample can be avoided in the detection process; the anti-interference performance is good, and cross reaction with rhodococcus equi, candida tropicalis and candida krusei does not exist.

The invention discloses a method for simultaneously determining the concentrations of Venoclarias, Selanisol, voriconazole and fluconazole in human plasma, and belongs to the technical field of drug analysis and treatment drug monitoring. The invention aims to solve the problem that the prior art is lack of a method for synchronously monitoring the blood concentration of four drugs of'vinca + Sanisole 'double-targeted chemotherapy and'voriconazole + fluconazole' antifungal scheme. The method is characterized by comprising the following steps: taking a plasma sample, precipitating protein through an internal standard solution and an organic solvent, and taking supernatant as a test solution; carrying out gradient elution by adopting a C18 chromatographic column and taking an aqueous solution containing formic acid and an organic solvent as mobile phases; detecting elution components by adopting an electrospray ionization source positive ion mode and a multi-reaction monitoring mode; and finally calculating the concentrations of the four drugs according to a detection result by an internal standard method. The method is mainly used for rapid and synchronous treatment drug monitoring when a clinical patient jointly uses the four drugs, and a basis is provided for accurate dose adjustment.

The application discloses application of cyanidin chloride or a pharmaceutical salt thereof in preparation of a drug for resisting drug-resistant fungi. The fungi are selected from drug-resistant Candida albicans. The application also provides application of cyanidin chloride or a pharmaceutical salt thereof in preparation of a drug-resistant fungus resisting reversal agent. The cyanidin chloride or the pharmaceutical salt thereof can be combined with fluconazole, a drug for resisting fungi, to improve the sensitivity of drug-resistant bacteria to fluconazole, realize the reversal of drug resistance, and resist fungi in a synergic way. Therefore, the cyanidin chloride or the pharmaceutical salt thereof can be used as the drug-resistant fungus resisting reversal agent.